[CAS NO. 1254472-97-3] Fezagepras sodium
PRODUCTS SPECIFICATIONS [1254472-97-3]
DESCRIPTION [1254472-97-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 228.26 |
| Molecular Formula | C13H17NaO2 |
| SMILES | O=C(O[Na])CC1=CC(CCCCC)=CC=C1 |
Summary
IC50 & Target
GPR40, GPR84 [1]
In Vitro
Fezagepras sodium (500 µM; 24 hours) inhibits TGF-β (10 ng/mL)-activated human hepatic stellate cells (HSCs) proliferation
[2]
.
Fezagepras sodium (250 or 500 µM; 24 hours) dose-dependently arrests HSCs at the G0/G1 phase without inducing apoptosis
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay [2]
| Cell Line: | HSCs |
| Concentration: | 250 or 500 µM |
| Incubation Time: | 24 hours |
| Result: | Inhibited TGF-β-activated HSC proliferation. TGF-β (10 ng/mL) increased HSC proliferation by 10%. |
Cell Cycle Analysis [2]
| Cell Line: | HSCs |
| Concentration: | 250 µM, 500 µM |
| Incubation Time: | 24 hours |
| Result: | Inhibited cell cycle progression. |
In Vivo
Fezagepras sodium (100 mg/kg/day; gavage from 8-20 weeks of age) markedly decreases hyperglycemia and markedly improvea glucose tolerance in type 2 diabetes eNOS -/- db/db mice [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Type 2 diabetes eNOS -/- db/db mice [1] |
| Dosage: | 100 mg/kg/day |
| Administration: | Given via daily gavage from 8-20 weeks |
| Result: | Compared with vehicle-treated mice, hyperglycemia was markedly decreased, and glucose tolerance was markedly improved. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT03081598 | Liminal BioSciences Ltd. |
Type 2 Diabetes Mellitus|Metabolic Syndrome
|
May 29, 2017 | Phase 2 |
| NCT02538536 | Liminal BioSciences Ltd. |
Idiopathic Pulmonary Fibrosis (IPF)
|
July 2015 | Phase 2 |
| NCT03637049 | Liminal BioSciences Ltd.|Celerion |
Healthy
|
July 17, 2018 | Phase 1 |
| NCT03184584 | Liminal BioSciences Ltd. |
Alström Syndrome
|
October 9, 2017 | Phase 2|Phase 3 |
| NCT02955888 | Liminal BioSciences Ltd. |
Cystic Fibrosis
|
January 3, 2017 | Phase 2 |
| NCT02739217 | Liminal BioSciences Ltd. |
Inflammation and Fibrosis|Diabetes
|
February 22, 2016 | Phase 2 |
| NCT02562573 | Liminal BioSciences Ltd. |
Type 2 Diabetes|Metabolic Syndrome
|
May 2015 | Phase 2 |
| NCT05349435 | Liminal BioSciences Ltd. |
Hyperammonemia
|
May 13, 2022 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : ≥ 100 mg/mL ( 438.10 mM )
DMSO : ≥ 64 mg/mL ( 280.38 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 4.3810 mL | 21.9048 mL | 43.8097 mL |
| 5 mM | 0.8762 mL | 4.3810 mL | 8.7619 mL |
| 10 mM | 0.4381 mL | 2.1905 mL | 4.3810 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 120 mg/mL (525.72 mM); Clear solution; Need ultrasonic
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (9.11 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (9.11 mM); Clear solution
References
- [1] Li Y, et al. Fatty acid receptor modulator PBI-4050 inhibits kidney fibrosis and improves glycemic control. JCI Insight. 2018 May 17;3(10). pii: 120365.
- [2] Grouix B, et al. PBI-4050 Reduces Stellate Cell Activation and Liver Fibrosis through Modulation of Intracellular ATP Levels and the Liver Kinase B1/AMP-Activated Protein Kinase/Mammalian Target of Rapamycin Pathway. J Pharmacol Exp Ther. 2018 Oct;367(1):